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Home >> Signaling Pathways >> Chromatin/Epigenetics >> HIF

HIF

Hypoxia inducible factors (HIFs) are heterodimeric proteins belonging to the basic helix-loop-helix-PAS (bHLH/PAS) family of transcription factors that mediate the primary transcriptional response to stress caused by hypoxia (accessible O2 level < 2%). HIFs are characterized by containing two subunits, including O2-labile α subunit (HIFα) and constitutively expressed β subnit (HIFβ). Mammalian HIFα consists of three isoforms, including HIF1α, HIF2α and HIF3α, which play an essential role in the regulation of HIF activity by O2 availability. Under normal O2 tension, HIFα is hydroxylated at the two conserved proline residues within the O2-dependent degradation (ODD) domain by prolylhydroxylase domain proteins (PHDs) and undergoes proteosomal degradation catalyzed by a complex formed by E3 ubiquitin ligase and the von Hippel-Lindau protein (pVHL); while, under hypoxia, HIFα stabilizes with PHDs being deactivated and hence induce transcription of genes with adaptive functions.

Products for  HIF

  1. Cat.No. Product Name Information
  2. GC69794 (Rac)-Arnebin 1

    (Rac)-β,β-Dimethylacrylalkannin; (Rac)-β,β-?Dimethylacrylshikonin

    (Rac)-Arnebin 1 is the racemic form of β,β-Dimethylacrylalkannin and/or β,β-Dimethylacrylshikonin. These compounds are naphthoquinones isolated from plants in the Lithospermum genus, with β,β-Dimethylacrylshikonin exhibiting anti-tumor activity.

     (Rac)-Arnebin 1 Chemical Structure
  3. GC65133 (S,R,S)-AHPC-C5-COOH

    VH032-C5-COOH

     (S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized?E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases. (S,R,S)-AHPC-C5-COOH Chemical Structure
  4. GC61949 1,4-DPCA ethyl ester 1,4-DPCA ethyl ester is the ethyl ester of 1,4-DPCA and can inhibit factor inhibiting HIF (FIH). 1,4-DPCA ethyl ester Chemical Structure
  5. GC16195 2,4-DPD

    2,4-Diethylpyridine dicarboxylate

     Diethyl pyridine-2,4-dicarb is a potent prolyl 4-hydroxylase-directed proinhibitor. 2,4-DPD Chemical Structure
  6. GC15084 2-Methoxyestradiol (2-MeOE2)

    2Hydroxyestradiol 2methyl ether, 2ME2, NSC 659853, Panzem

     2-Methoxyestradiol (2-MeOE2/2-Me) is an HIF-1α inhibitor. 2-Methoxyestradiol (2-MeOE2) Chemical Structure
  7. GC14282 3-acetyl-11-keto-β-Boswellic Acid

    3-O-acetyl-11-keto-β-Boswellic acid,AKBA

     3-acetyl-11-keto-β-Boswellic Acid (Acetyl-11-keto-β-boswellic acid) is an active triterpenoid compound from the extract of Boswellia serrate and a novel Nrf2 activator. 3-acetyl-11-keto-β-Boswellic Acid Chemical Structure
  8. GC35230 Acetylarenobufagin Acetylarenobufagin is a steroidal hypoxia inducible factor-1 (HIF-I) modulator. Acetylarenobufagin Chemical Structure
  9. GC32083 Acriflavine Acriflavine is a fluorescent dye for labeling high molecular weight RNA. Acriflavine Chemical Structure
  10. GC62354 Acriflavine hydrochloride Acriflavine hydrochloride (Acriflavinium chloride hydrochloride) is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine hydrochloride Chemical Structure
  11. GC12487 Adaptaquin

    HIF prolyl hydroxylase inhibitor

     HIF-prolyl hydroxylase-2 (PHD2) inhibitor Adaptaquin Chemical Structure
  12. GC33416 AFP464

    NSC710464 free base

     AFP464 (NSC710464 free base), is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator. AFP464 Chemical Structure
  13. GC73864 AFP464 dihydrochloride

    NSC710464 dihydrochloride

     AFP464 (didrochloride) (NSC710464 (didrochloride)) is the drochloride form of AFP464 and is a potent HIF-1α inhibitor with an IC50 value of 0.25 μM. AFP464 dihydrochloride Chemical Structure
  14. GC62277 AKB-6899 Ro24-7429 is a potent and orally active HIV-1 transactivator protein Tat antagonist. Ro24-7429 is also a runt-related transcription factor 1 (RUNX1) inhibitor. Ro24-7429 has anti-HIV, antifibrotic and anti-inflammatory effects. AKB-6899 Chemical Structure
  15. GC42785 Amifostine (hydrate)

    Ethyol, WR 2721

     Amifostine (hydrate) (WR2721 trihydrate) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine (hydrate) selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine (hydrate) is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine (hydrate) protects cells from damage by scavenging oxygen-derived free radicals. Amifostine (hydrate) reduces renal toxicity and has antiangiogenic action. Amifostine (hydrate) Chemical Structure
  16. GC12698 BAY 87-2243 A HIF-1 inhibitor,potent and selective BAY 87-2243 Chemical Structure
  17. GC70471 BNS BNS is a cell penetrant, potent and selective PHD2 (prolyl-hydroxylase 2) inhibitor. BNS Chemical Structure
  18. GC17405 Chetomin

    NSC 289491

     An inhibitor of HIF signaling Chetomin Chemical Structure
  19. GN10518 Chitosamine hydrochloride

    D-(+)-Glucosamine, GlcN, NSC 234443, NSC 758

     Chitosamine hydrochloride Chemical Structure
  20. GN10308 Chlorogenic acid

    3OCaffeoylquinic acid, Heriguard, NSC 407296

     Chlorogenic acid is a potent neuroprotective agent and also has antiviral,antifungal antioxidant and antitumor properties. CGA is also involved in regulating glucose and lipid metabolism and improving insulin sensitivity. Chlorogenic acid Chemical Structure
  21. GC74310 Cyclo(CKLIIF) TFA Cyclo CKLIIF is a dual inhibitor for poxia inducible factor (HIF) 1 and 2, with affinity for HIF1-α and HIF2-α PAS-B domains KD of 2.6 and 2.2 μM, respectively. Cyclo(CKLIIF) TFA Chemical Structure
  22. GC16647 Daprodustat(GSK1278863)

    GSK1278863

     Daprodustat(GSK1278863) (GSK1278863) is an orally active hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor being developed for the treatment of anemia associated with chronic kidney disease. Daprodustat(GSK1278863) Chemical Structure
  23. GC68955 Deferoxamine

    Deferoxamine (Deferoxamine B) is an iron chelator (binding Fe(III) and many other metal cations), widely used to reduce the accumulation and deposition of iron in tissues. 

     Deferoxamine Chemical Structure
  24. GC31230 Dencichin (Dencichine) Dencichin is a non-protein amino acid originally extracted from Panax notoginseng, and can inhibit HIF-prolyl hydroxylase-2 (PHD-2) activity. Dencichin (Dencichine) Chemical Structure
  25. GC38767 Deoxyshikonin A natural products with anti-tumor activity Deoxyshikonin Chemical Structure
  26. GC32449 Desidustat

    P 1560, β-Zearalanol, β-Zearanol

     An inhibitor of HIF-PH Desidustat Chemical Structure
  27. GC73945 DYB-03 DYB-03 is an oral active HIF-1α/EZH2 inhibitor. DYB-03 Chemical Structure
  28. GC18236 Echinomycin

    Antibiotic A 654I； NSC 13502； NSC 526417； Quinomycin A； SK 302B

     An inhibitor of HIF1mediated gene transcription Echinomycin Chemical Structure
  29. GC33043 EL-102 EL-102 is a hypoxia-induced factor 1 (Hif1α) inhibitor. EL-102 induces apoptosis, inhibits tubulin polymerisation and shows activities against prostate cancer. EL-102 can be used for the research of cancer. EL-102 Chemical Structure
  30. GC33634 Enarodustat (JTZ-951)

    JTZ-951

     Enarodustat (JTZ-951) is a potent and orally active hypoxia-inducible factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM. Enarodustat (JTZ-951) Chemical Structure
  31. GC33170 ENMD-119 (ENMD 1198)

    IRC-110160

     ENMD-119 (ENMD 1198) (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-119 (ENMD 1198) is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization. ENMD-119 (ENMD 1198) Chemical Structure
  32. GC61669 Ethyl 3,4-dihydroxybenzoate Ethyl 3,4-dihydroxybenzoate (Ethyl protocatechuate), an antioxidant, is a prolyl-hydroxylase inhibitor found in the testa of peanut seeds. Ethyl 3,4-dihydroxybenzoate Chemical Structure
  33. GC13139 FG-4592 (ASP1517)

    ASP1517, FG-4592

    FG-4592, as an oral bioavailable hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitor, can promote coordinated erythropoiesis through HIF-mediated transcription.

     FG-4592 (ASP1517) Chemical Structure
  34. GC16638 FG2216

    IOX3, YM-311

     HIF-prolyl hydroxylase inhibitor FG2216 Chemical Structure
  35. GC50537 FM19G11 A HIF α-subunit inhibitor FM19G11 Chemical Structure
  36. GC38044 Fraxinellone Fraxinellone Chemical Structure
  37. GC30263 Glucosamine (D-Glucosamine) Glucosamine (D-Glucosamine) (D-Glucosamine (D-Glucosamine)) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement. Glucosamine (D-Glucosamine) Chemical Structure
  38. GN10669 Glucosamine sulfate Glucosamine sulfate Chemical Structure
  39. GC34595 GN44028 A HIF-1 inhibitor GN44028 Chemical Structure
  40. GC40918 Gramicidin A Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. Gramicidin A Chemical Structure
  41. GC39146 HIF-1 inhibitor-1 An inhibitor of HIF-1 signaling HIF-1 inhibitor-1 Chemical Structure
  42. GC66464 HIF-1α-IN-2 HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation. HIF-1α-IN-2 Chemical Structure
  43. GC72867 HIF-1α-IN-2 hydrochloride HIF-1α-IN-2 drochloride is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 hydrochloride Chemical Structure
  44. GC73346 HIF-1α-IN-4 HIF-1α-IN-4 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-4 Chemical Structure
  45. GC73347 HIF-1α-IN-5 HIF-1α-IN-5 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-5 Chemical Structure
  46. GC73339 HIF-1/2α-IN-2 HIF-1/2α-IN-2 is an inhibitor of HIF-1/2α. HIF-1/2α-IN-2 Chemical Structure
  47. GC69226 HIF-2α agonist 2

    HIF-2α agonist 2 (compound 10) is a HIF-2α activator with an EC50 value of 1.68 μM at a dose of 20 μM. HIF-2α agonist 2 has no cytotoxicity on 786-O-HRE-Luc cells. It can be used for oxygen metabolism research.

     HIF-2α agonist 2 Chemical Structure
  48. GC62584 HIF-2α-IN-2 HIF-2α-IN-2 is a hypoxia-inducible factors (HIF-2α) inhibitor extracted from patent WO2015035223A1, Compound 232, has an IC50 of 16 nM in scintillation proximity assay (SPA). HIF-2α-IN-2 Chemical Structure
  49. GC62418 HIF-2α-IN-3 HIF-2α-IN-3, an allosteric inhibitor of hypoxia inducible factor-2α (HIF-2α), exhibits an IC50 of 0.4 μM and a KD of 1.1 μM. Anticancer agent. HIF-2α-IN-3 Chemical Structure
  50. GC63678 HIF-2α-IN-4 HIF-2α-IN-4 is a potent inhibitor of hypoxia inducible factor-2α (HIF-2α) translation, with an IC50 of 5 μM. HIF-2α-IN-4 decreases both constitutive and hypoxia-induced HIF-2α protein expression. HIF-2α-IN-4 links its 5'UTR iron-responsive element to oxygen sensing. HIF-2α-IN-4 Chemical Structure
  51. GC69225 HIF-2α-IN-8

    HIF-2α-IN-8 is an effective orally active inhibitor of HIF2α with IC50 values of 9, 37, and 246 nM for HIF2α SPA, HIF2α iScript, and HIF2α HRE RGA respectively. It has anti-tumor activity.

     HIF-2α-IN-8 Chemical Structure
  52. GC31358 HIF-2α-IN-1 HIF-2α-IN-1 is a HIF-2α inhibitor has an IC50 of less than 500 nM in HIF-2α scintillation proximity assay. HIF-2α-IN-1 Chemical Structure
  53. GC69227 HIF-IN-1

    HIF-IN-1 (Compound 3c) is a hypoxia-inducible factor (HIF-1) inhibitor. HIF-IN-1 inhibits the aggregation of HIF-1α protein without affecting the level of HIF-1α mRNA. HIF-IN-1 has no significant cytotoxicity.

     HIF-IN-1 Chemical Structure
  54. GC67941 HIF-PHD-IN-1 HIF-PHD-IN-1 Chemical Structure
  55. GC65570 HIF1-IN-3 HIF1-IN-3 (compound F4) is a potent HIF1 inhibitor with an EC50 value of 0.9 μM. HIF1-IN-3 can be used for researching anticancer. HIF1-IN-3 Chemical Structure
  56. GC11767 Hydralazine HCl

    1-Hydrazinophthalazine

     Hydralazine HCl is a orally active antihypertensive agent, reduces peripheral resistance directly by relaxing the smooth muscle cell layer in arterial vessel. Hydralazine HCl Chemical Structure
  57. GC60919 Hydroxycitric acid tripotassium hydrate Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia. Hydroxycitric acid tripotassium hydrate Chemical Structure
  58. GC32948 IDF-11774 A novel HIF-1 inhibitor IDF-11774 Chemical Structure
  59. GC13018 IOX2(Glycine) A selective PHD2 inhibitor IOX2(Glycine) Chemical Structure
  60. GC12255 IOX4 PHD2 inhibitor IOX4 Chemical Structure
  61. GC73813 IOX5 IOX5 is a selective prolyl droxylases (PHD) inhibitor. IOX5 Chemical Structure
  62. GC63828 Izilendustat Izilendustat is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2). Izilendustat Chemical Structure
  63. GC15379 JNJ-42041935

    HIF-PHD Inhibitor II

     Hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor JNJ-42041935 Chemical Structure
  64. GC13141 KC7F2 An inhibitor of HIF-1a protein synthesis KC7F2 Chemical Structure
  65. GC32724 LW6 (HIF-1α inhibitor)

    Hypoxia-Inducible Factor1α Inhibitor

     LW6 is a hypoxia-inducing factor 1(HIF) inhibitor, which effectively inhibits HIF-1α accumulation by degrading HIF-1α, but does not affect HIF-1A mRNA level during hypoxia. LW6 (HIF-1α inhibitor) Chemical Structure
  66. GC64945 M1001 M1001 is a weak hypoxia-inducible factor-2α (HIF-2α) agonist. M1001 can bind to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 can be used in chronic kidney disease research. M1001 Chemical Structure
  67. GC65046 M1002 M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist, and can enhance the expression of HIF-2 target genes. M1002 shows synergy with prolyl-hydroxylase domain (PHD) inhibitors. M1002 Chemical Structure
  68. GC19251 MK-8617 MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2. MK-8617 Chemical Structure
  69. GC14319 ML 228

    CID-46742353

     A HIF pathway activator ML 228 Chemical Structure
  70. GC10046 Molidustat (BAY85-3934)

    Molidustat

     Molidustat (BAY85-3934) (BAY 85-3934) is a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with mean IC50 values of 480 nM for PHD1, 280 nM for PHD2, and 450 nM for PHD3. Molidustat (BAY85-3934) Chemical Structure
  71. GC62406 Moracin O Moracin O is a 2-arylbenzofuran isolated from the Mori Cortex Radicis. Moracin O Chemical Structure
  72. GC69488 Moracin P

    Moracin P is a 2-arylbenzofuran isolated from Mori Cortex Radicis. It exhibits strong in vitro inhibitory activity against hypoxia-inducible factor (HIF-1). Moracin P reduces the production of reactive oxygen species (ROS) induced by oxygen-glucose deprivation (OGD). Moracin P has neuroprotective and anti-inflammatory effects.

     Moracin P Chemical Structure
  73. GC17358 Octyl-α-ketoglutarate

    α-KG octyl ester

     prolyl hydroxylases (PHD) activator Octyl-α-ketoglutarate Chemical Structure
  74. GC12821 Oltipraz

    NSC 347901, RP 35972

     Nrf2 activator;An antischistosomal agent Oltipraz Chemical Structure
  75. GC41625 Oroxylin A

    6-Methoxybaicalein

    Oroxylin A is a flavonoid that has been found in S.

     Oroxylin A Chemical Structure
  76. GN10452 Paeoniflorin

    NSC 178886

     Paeoniflorin Chemical Structure
  77. GC64584 PHD-1-IN-1 PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM. PHD-1-IN-1 Chemical Structure
  78. GC41572 PRLX-93936

    PRLX-93936 is an analog of erastin that has antitumor activity.

     PRLX-93936 Chemical Structure
  79. GC72899 PRLX-93936 dihydrochloride PRLX-93936 didrochloride (Compound 16) is a HIF-1α inhibitor with anticancer activity. PRLX-93936 dihydrochloride Chemical Structure
  80. GC32680 PT-2385 PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM. PT-2385 Chemical Structure
  81. GC65333 PT2399 PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo. PT2399 Chemical Structure
  82. GC37034 PT2977

    PT2977; MK-6482

     PT2977 (PT2977) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. PT2977, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. PT2977 is a potential treatment for clear cell renal cell carcinoma (ccRCC). PT2977 Chemical Structure
  83. GC15594 PX 12

    IV-2

     An irreversible inhibitor of thioredoxin-1 PX 12 Chemical Structure
  84. GC11031 PX-478 2HCl

    PX-478 is a selective inhibitor that suppresses constitutive and hypoxia-induced HIF-1α levels.

     PX-478 2HCl Chemical Structure
  85. GC37066 Rac-PT2399 A potent and specific HIF-2α inhibitor Rac-PT2399 Chemical Structure
  86. GC49190 Roxadustat-d5 An internal standard for the quantification of roxadustat Roxadustat-d5 Chemical Structure
  87. GC69956 Steppogenin

    Steppogenin is an effective inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. Steppogenin can be used for research on angiogenesis-related diseases such as solid tumors.

     Steppogenin Chemical Structure
  88. GC32876 SYP-5 A HIF-1 inhibitor SYP-5 Chemical Structure
  89. GC50211 TAT-cyclo-CLLFVY Selective HIF-1 dimerization inhibitor TAT-cyclo-CLLFVY Chemical Structure
  90. GC50128 TC-S 7009 High affinity and selective HIF-2α inhibitor TC-S 7009 Chemical Structure
  91. GC32945 THS-044 THS-044 binding stabilizes the HIF2α PAS-B folded state, for regulating HIF2 activity in endogenous and clinical settings. THS-044 Chemical Structure
  92. GC32228 Tilorone dihydrochloride

    NSC 143969

     An interferon-inducing antiviral agent Tilorone dihydrochloride Chemical Structure
  93. GC40555 Tiopronin

    BRN 1859822, (±)-Tiopronin

     Tiopronin is an antioxidant that has diverse biological activities. Tiopronin Chemical Structure
  94. GC91083 Tiopronin-Cysteine Disulfide

    A metabolite of tiopronin

     Tiopronin-Cysteine Disulfide Chemical Structure
  95. GC49062 Tiopronin-d3

    (±)-Tiopronin-d3

     An internal standard for the quantification of tiopronin Tiopronin-d3 Chemical Structure
  96. GC37801 TM6089 TM6089 is a unique Prolyl Hydroxylase (PHD) inhibitor which stimulates HIF activity without iron chelation and induces angiogenesis and exerts organ protection against ischemia. TM6089 Chemical Structure
  97. GC31498 TP0463518

    TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor

     TP0463518 Chemical Structure
  98. GC64001 TRC160334 TRC160334 is a hypoxia-inducible factor (HIF) hydroxylase inhibitor. TRC160334 Chemical Structure
  99. GC16811 Vadadustat

    AKB6548, PG-1016548

     HIF-PH inhibitor Vadadustat Chemical Structure
  100. GC37889 VCE-004.8

    VCE-?004.8

     VCE-004.8 (VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist. VCE-004.8 Chemical Structure
  101. GC61863 Verucopeptin Verucopeptin is a potent?HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity?by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR)?cancers and can be used for cancer research. Verucopeptin Chemical Structure

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